The present invention relates to novel isoquinoline derivatives and pharmaceutically acceptable salts thereof. More specifically, the present invention relates to isoquinolyl guanidinobenzoate derivatives and they have application as protease inhibitors, in particular as antitrypsin agents. Furthermore, most of 5-hydroxyisoquinoline derivatives described in this invention, are new compounds and are useful as intermediates for the preparation of the isoquinolyl guanidinobenzoate derivatives.
JP No. 2107/74, U.S. Pat. No. 3,751,447 and Ger. Pat. No. 2050484 claim a series of guanidinocaproate. JP No. 1063/86, Eur. Pat. No. 48433 and U.S. Pat. No. 4,454,338 claim a series of guanidinobenzoate as useful protease inhibitors and anti-complementary agents. JP No. 89640/77, Ger. Pat. No. 2548886 and U.S. Pat. No. 4,021,472 claim a series of guanidinobenzoates as useful protease inhibitors.